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PE20141204A1 - NOVEL COMPOUNDS AS INHIBITORS OF DIACILGLICEROL ACILTRANSFERASE - Google Patents

NOVEL COMPOUNDS AS INHIBITORS OF DIACILGLICEROL ACILTRANSFERASE

Info

Publication number
PE20141204A1
PE20141204A1 PE2013002531A PE2013002531A PE20141204A1 PE 20141204 A1 PE20141204 A1 PE 20141204A1 PE 2013002531 A PE2013002531 A PE 2013002531A PE 2013002531 A PE2013002531 A PE 2013002531A PE 20141204 A1 PE20141204 A1 PE 20141204A1
Authority
PE
Peru
Prior art keywords
oxo
diacilglicerol
aciltransferase
inhibitors
novel compounds
Prior art date
Application number
PE2013002531A
Other languages
Spanish (es)
Inventor
Donghui Qin
Mui Cheung
Hemant Joshi
Raghuram Tangirala
Sridhar Reddy Bethi
Original Assignee
Glaxosmithkline Ip No 2 Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Glaxosmithkline Ip No 2 Ltd filed Critical Glaxosmithkline Ip No 2 Ltd
Publication of PE20141204A1 publication Critical patent/PE20141204A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

SE REFIERE A COMPUESTOS INHIBIDORES DE DIACILGLICEROL ACILTRANSFERASA DE FORMULA (I) EN DONDE R1 ES UN SISTEMA DE ANILLO BICICLICO QUE CONSTIENE 9 A 11 MIEMBROS DEL ANILLO INCLUYENDO 1 A 4 HETEROATOMOS, ENTRE OTROS; R2 Y R3 ES INDEPENDIENTEMENTE H, ALQUILO C1-C6, HALO, HIDROXILO, ENTRE OTROS; m ES 0-2. SON COMPUESTOS PREFERIDOS EL ACIDO 2-(6-{4-AMINO-5-OXO-5H,6H,7H,8H-PIRIMIDO[5,4-F][1,4]OXAZEPIN-6-IL}-1-OXO-1,2,3,4-TETRAHIDROISOQUINOLIN-2-IL)ACETICO, 2-(6-{4-AMINO-5-OXO-5H,6H,7H,8H-PIRIMIDO[5,4-F][1,4]OXAZEPIN-6-IL}-2-OXO-1,2,3,4- TETRAHIDROISOQUINOLIN-1-IL)ACETATO DE ETILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA QUE ES UTIL PARA EL TRATAMIENTO DE TRASTORNOS RELACIONADOS CON LA OBESIDADREFERS TO INHIBITING COMPOUNDS OF DIACILGLICEROL ACILTRANSFERASE OF FORMULA (I) WHERE R1 IS A BICYCLE RING SYSTEM CONSISTING 9 TO 11 MEMBERS OF THE RING INCLUDING 1 TO 4 HETEROATOMS, AMONG OTHERS; R2 AND R3 IS INDEPENDENTLY H, C1-C6 ALKYL, HALO, HYDROXYL, AMONG OTHERS; m IS 0-2. PREFERRED COMPOUNDS ARE THE ACID 2- (6- {4-AMINO-5-OXO-5H, 6H, 7H, 8H-PYRIMIDO [5,4-F] [1,4] OXAZEPIN-6-IL} -1-OXO -1,2,3,4-TETRAHYDROISOQUINOLIN-2-IL) ACETIC, 2- (6- {4-AMINO-5-OXO-5H, 6H, 7H, 8H-PYRIMIDO [5,4-F] [1, 4] OXAZEPIN-6-IL} -2-OXO-1,2,3,4- TETRAHYDROISOQUINOLIN-1-IL) ETHYL ACETATE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION THAT IS USEFUL FOR THE TREATMENT OF OBESITY-RELATED DISORDERS

PE2013002531A 2011-05-20 2012-05-18 NOVEL COMPOUNDS AS INHIBITORS OF DIACILGLICEROL ACILTRANSFERASE PE20141204A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1452DE2011 2011-05-20
US201161503728P 2011-07-01 2011-07-01

Publications (1)

Publication Number Publication Date
PE20141204A1 true PE20141204A1 (en) 2014-10-05

Family

ID=47217645

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2013002531A PE20141204A1 (en) 2011-05-20 2012-05-18 NOVEL COMPOUNDS AS INHIBITORS OF DIACILGLICEROL ACILTRANSFERASE

Country Status (34)

Country Link
US (4) US8859536B2 (en)
EP (1) EP2710013B1 (en)
JP (1) JP5844456B2 (en)
KR (1) KR101919080B1 (en)
CN (1) CN103703009B (en)
AU (1) AU2012259044B2 (en)
BR (1) BR112013029935B1 (en)
CA (1) CA2836669C (en)
CO (1) CO6811855A2 (en)
CR (1) CR20130602A (en)
CY (1) CY1118188T1 (en)
DK (1) DK2710013T3 (en)
DO (1) DOP2013000272A (en)
EA (1) EA023030B1 (en)
ES (1) ES2588748T3 (en)
HK (1) HK1194738A1 (en)
HR (1) HRP20161089T1 (en)
HU (1) HUE028870T2 (en)
IL (1) IL229488A (en)
LT (1) LT2710013T (en)
MA (1) MA35185B1 (en)
ME (1) ME02479B (en)
MX (1) MX346494B (en)
MY (1) MY184553A (en)
PE (1) PE20141204A1 (en)
PL (1) PL2710013T3 (en)
PT (1) PT2710013T (en)
RS (1) RS55006B1 (en)
SG (1) SG195044A1 (en)
SI (1) SI2710013T1 (en)
SM (1) SMT201600328B (en)
UA (1) UA111360C2 (en)
WO (1) WO2012162129A1 (en)
ZA (1) ZA201308664B (en)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PE20141204A1 (en) 2011-05-20 2014-10-05 Glaxosmithkline Ip No 2 Ltd NOVEL COMPOUNDS AS INHIBITORS OF DIACILGLICEROL ACILTRANSFERASE
LT2922551T (en) 2012-11-23 2019-02-11 Glaxosmithkline Llc Novel compounds as diacylglycerol acyltransferase inhibitors
US9796729B2 (en) 2012-11-23 2017-10-24 Glaxosmithkline Llc Compounds as diacylglycerol acyltransferase inhibitors
WO2014081996A1 (en) * 2012-11-23 2014-05-30 Glaxosmithkline Llc Novel compounds as diacylglycerol acyltransferase inhibitors
CN103524431B (en) * 2013-09-24 2016-01-13 西安交通大学 3-benzyl-4-quianzolinones and synthetic method thereof and application
WO2015049667A1 (en) 2013-10-03 2015-04-09 Glaxosmithkline Intellectual Property (No.2) Limited Novel compound as a diacylglycerol acyltransferase inhibitor
WO2015049668A1 (en) 2013-10-03 2015-04-09 Glaxosmithkline Intellectual Property (No.2) Limited Novel compound as a diacylglycerol acyltransferase inhibitor
CN103880757B (en) * 2014-04-15 2016-02-24 上海毕得医药科技有限公司 A kind of synthetic method of 5-hydroxy pyrimidine-2-carboxylic acid
WO2016181409A1 (en) 2015-05-11 2016-11-17 Cadila Healthcare Limited Saroglitazar magnesium for the treatment of chylomicronemia syndrome -
WO2017064635A2 (en) 2015-10-14 2017-04-20 Cadila Healthcare Limited Pyrrole compound, compositions and process for preparation thereof
CN105732461A (en) * 2016-02-03 2016-07-06 常州工程职业技术学院 Preparation method of 5-methoxy group-6-halogenated indole
CN106083707B (en) * 2016-06-01 2018-10-26 温州大学 A kind of synthetic method of asymmetric heteroaryl thioether
CN107619928B (en) * 2016-07-15 2020-08-07 中国科学院上海有机化学研究所 Extraction composition, extraction system and application thereof
CN107619932B (en) * 2016-07-15 2020-08-07 中国科学院上海有机化学研究所 Extraction composition, extraction system and application thereof
RU2706655C1 (en) * 2019-01-28 2019-11-19 Акционерное общество "Гознак" (АО "Гознак") Polymer-containing composite protected article

Family Cites Families (7)

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US20090036425A1 (en) * 2007-08-02 2009-02-05 Pfizer Inc Substituted bicyclolactam compounds
SG172259A1 (en) * 2008-12-19 2011-07-28 Genentech Inc Heterocyclic compounds and methods of use
TW201038580A (en) * 2009-02-02 2010-11-01 Pfizer 4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl derivatives
AU2010226826A1 (en) * 2009-03-18 2011-10-13 Merck Sharp & Dohme Corp. Bicyclic compounds as inhibitors of diacylglycerol acyltransferase
EP2421854B1 (en) * 2009-04-24 2014-07-23 F.Hoffmann-La Roche Ag Inhibitors of bruton's tyrosine kinase
PE20141204A1 (en) 2011-05-20 2014-10-05 Glaxosmithkline Ip No 2 Ltd NOVEL COMPOUNDS AS INHIBITORS OF DIACILGLICEROL ACILTRANSFERASE
US9796729B2 (en) 2012-11-23 2017-10-24 Glaxosmithkline Llc Compounds as diacylglycerol acyltransferase inhibitors

Also Published As

Publication number Publication date
KR101919080B1 (en) 2018-11-16
US9040517B2 (en) 2015-05-26
UA111360C2 (en) 2016-04-25
JP5844456B2 (en) 2016-01-20
US20140080809A1 (en) 2014-03-20
ME02479B (en) 2017-02-20
IL229488A (en) 2016-04-21
CO6811855A2 (en) 2013-12-16
US9540400B2 (en) 2017-01-10
CN103703009B (en) 2016-08-17
ZA201308664B (en) 2015-02-25
MA35185B1 (en) 2014-06-02
RS55006B1 (en) 2016-11-30
MY184553A (en) 2021-04-02
EA201391737A1 (en) 2014-04-30
SMT201600328B (en) 2016-11-10
PL2710013T3 (en) 2017-08-31
US9273069B2 (en) 2016-03-01
SI2710013T1 (en) 2016-10-28
HUE028870T2 (en) 2017-01-30
US8859536B2 (en) 2014-10-14
BR112013029935B1 (en) 2020-12-15
EA023030B1 (en) 2016-04-29
CN103703009A (en) 2014-04-02
DOP2013000272A (en) 2014-05-15
NZ617991A (en) 2015-06-26
EP2710013A4 (en) 2014-11-05
CA2836669A1 (en) 2012-11-29
HK1194738A1 (en) 2014-10-24
EP2710013A1 (en) 2014-03-26
CY1118188T1 (en) 2017-06-28
IL229488A0 (en) 2014-01-30
MX2013013566A (en) 2014-01-08
US20140378434A1 (en) 2014-12-25
CR20130602A (en) 2014-08-13
US20160200736A1 (en) 2016-07-14
HRP20161089T1 (en) 2016-10-21
SG195044A1 (en) 2013-12-30
MX346494B (en) 2017-03-21
BR112013029935A2 (en) 2016-09-20
JP2014517839A (en) 2014-07-24
AU2012259044B2 (en) 2015-09-17
US20150225425A1 (en) 2015-08-13
PT2710013T (en) 2016-09-28
ES2588748T3 (en) 2016-11-04
EP2710013B1 (en) 2016-06-29
CA2836669C (en) 2019-03-19
AU2012259044A1 (en) 2013-12-12
KR20140045415A (en) 2014-04-16
LT2710013T (en) 2016-09-12
WO2012162129A1 (en) 2012-11-29
DK2710013T3 (en) 2016-09-26

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